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Drug intelligence / Profile preview
apatinib + irinotecan
- Development stage
- Phase 3
- Lead developer
- Hengrui Therapeutics
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Apatinib + irinotecan is a combination therapy that pairs two distinct medications with complementary mechanisms of action. Apatinib is a small-molecule tyrosine kinase inhibitor specifically targeting vascular endothelial growth factor receptor-2 (VEGFR-2), functioning as an antiangiogenic agent that inhibits tumor blood vessel formation[1]. Irinotecan is a topoisomerase I inhibitor that prevents DNA replication in cancer cells[7]. This combination has been studied in various cancer types, with particularly promising results in advanced gastric adenocarcinoma (GAC), gastroesophageal junction adenocarcinoma (GEJA), esophageal squamous cell carcinoma (ESCC), and small cell esophageal carcinoma (SCEC)[1][2][3]. The rationale behind combining these agents is to simultaneously target tumor angiogenesis and DNA replication, potentially overcoming resistance mechanisms and enhancing therapeutic efficacy.
- Brand names
- Aivita
- Other names
- Apatinib mesylateIrinotecan hydrochloride
02
Targets
TOP1 (DNA Topoisomerase I)VEGFR2 (Vascular endothelial growth factor receptor 2)
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